1. GPCR/G Protein
    Neuronal Signaling
  2. Opioid Receptor
  3. BMS-986122

BMS-986122 

Cat. No.: HY-120645 Purity: ≥98.0%
Handling Instructions

BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [35S]GTPγS binding in mouse brain membranes.

For research use only. We do not sell to patients.

BMS-986122 Chemical Structure

BMS-986122 Chemical Structure

CAS No. : 313669-88-4

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Description

BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [35S]GTPγS binding in mouse brain membranes[1][2].

In Vitro

BMS-986122 increases β-arrestin recruitment stimulated by endomorphin 1 (EC50=3 μM) in U2OS-OPRM1 human osteosarcoma cells expressing μ-opioid receptors.BMS-986122 potentiates endomorphin 1-induced inhibition of forskolin-stimulated adenylyl cyclase activity in CHO cells expressing human recombinant μ-opioid receptors (EC50=8.9 μM). BMS-986122 potentiates DAMGO-mediated [35S]GTPγS binding in mouse brain membranes and appears to be, at least in part, a positive affinity modulator of the μ-opioid receptor for DAMGO binding[1].
BMS-986122 enhances the ability of the endogenous opioid Methionine-enkephalin (Met-Enk) to stimulate G protein activity in mouse brain homogenates without activity on its own and to enhance G protein activation to a greater extent than β-arrestin recruitment in CHO cells expressing human mu-opioid receptors. BMS-986122 increases the potency of Met-Enk to inhibit GABA release in the periaqueductal gray, an important site for antinociception[2].
BMS-986122 is selective for µ-OR and has no detectable activity at the closely related δ-OR. BMS-986122 is a silent allosteric modulator at δ-OR and κ-OR[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

448.78

Formula

C₁₆H₁₅BrClNO₃S₂

CAS No.
SMILES

O=S(N1C(C2=CC=C(OC)C(Br)=C2)SCC1)(C3=CC=C(Cl)C=C3)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
References

Purity: ≥98.0%

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Keywords:

BMS-986122BMS986122BMS 986122Opioid ReceptorpositiveallostericmodulatorGproteinβ-arrestinrecruitmentadenylylcyclaseInhibitorinhibitorinhibit

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BMS-986122
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